Studies on 5-fluoro-.ALPHA.-methyltryptamine and p-chloro-.BETA.-methylphenethylamine: Determination of the MAO-A or MAO-B selective inhibition in vitro. | Zendy

Hiroyasu Kinemuchi | Zendy; Yuichiro Arai | Zendy; Yoshie Toyoshima | Zendy; Takeshi Tadano | Zendy; Kensuke Kisara | Zendy

Open Access

Studies on 5-fluoro-.ALPHA.-methyltryptamine and p-chloro-.BETA.-methylphenethylamine: Determination of the MAO-A or MAO-B selective inhibition in vitro.

Author(s) -

Hiroyasu Kinemuchi,

Yuichiro Arai,

Yoshie Toyoshima,

Takeshi Tadano,

Kensuke Kisara

Publication year - 1988

Publication title -

the japanese journal of pharmacology

Language(s) - English

Resource type - Journals

eISSN - 1347-3506

pISSN - 0021-5198

DOI - 10.1254/jjp.46.197

Subject(s) - in vitro , in vivo , non competitive inhibition , chemistry , stereochemistry , alpha (finance) , inhibitory postsynaptic potential , pharmacology , biochemistry , enzyme , biology , medicine , surgery , construct validity , microbiology and biotechnology , patient satisfaction

To further clarify highly MAO-A- or -B-selective inhibitory properties of 5-fluoro-alpha-methyltryptamine (5-FMT) and p-chloro-beta-methylphenethylamine (p-CMPEA), we determined the types and K1 values of inhibition of rat brain MAO-A and -B activity in vitro. The kinetic data obtained showed that 5-FMT is a competitive MAO-A-selective inhibitor with about a 18,000-fold higher sensitivity than MAO-B. In contrast, p-CMPEA is a competitive MAO-B-selective inhibitor with about a 620-fold higher sensitivity. Based on the present findings of highly MAO-A- or -B-selective inhibition, these two compounds might prove to be of value in in vivo studies.

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